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Histone lysine specific demethylase 1 inhibitors

Samir Mehndiratta1,2, Jing-Ping Liou1

  • 1School of Pharmacy , College of Pharmacy , Taipei Medical University , Taiwan . Email: jpl@tmu.edu.tw ; Tel: +886 2 2736 1661 ext 6130.

RSC Medicinal Chemistry
|January 22, 2021
PubMed

Insights

Lysine Specific Demethylase 1 (LSD1) is crucial in biological processes and linked to cancers. Recent research focuses on developing LSD1 inhibitors for treating acute myeloid leukemia (AML), with some now in clinical trials.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Lysine Specific Demethylase 1 (LSD1) is vital for cellular functions.
  • Overexpression of LSD1 is implicated in various cancers.
  • LSD1 is a promising therapeutic target for acute myeloid leukemia (AML).

Purpose of the Study:

  • To review recent advancements in the design and evaluation of LSD1 inhibitors.
  • To highlight the therapeutic potential of targeting LSD1 in malignancies, particularly AML.
  • To provide an overview of LSD1-targeting pharmacophores developed in recent years.

Main Methods:

  • Literature review of scientific publications and clinical trial data.
  • Analysis of diverse chemical architectures of LSD1 inhibitors.
  • Summary of research developments in LSD1 pharmacophores.

Main Results:

  • Numerous LSD1 inhibitors with varied chemical structures have been synthesized and evaluated.
  • Several LSD1 inhibitors have progressed to clinical trials for AML treatment.
  • Recent research has identified novel LSD1-targeting pharmacophores.

Conclusions:

  • LSD1 inhibitors represent a promising therapeutic strategy for AML.
  • Continued research into LSD1 pharmacophores may yield new cancer treatments.
  • The clinical evaluation of LSD1 inhibitors is ongoing and shows potential.

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